Target fishing

We offer a sophisticated chemical derivatization based affinity chromatography technology for selectivity profiling and off- target identification of kinase inhibitors. We perform delicate chemistry to accomplish the proper chemical modification of the kinase inhibitor to maintain its kinase inhibitory activity.

The KinaTor technology is offered on a service basis by Kinaxo (Martinsried, Germany). Vichem is generating the functional derivatives, which are being used for immobilization. The derivatization service combines structural and synthetic know how and can be offered to interested partners on a non-exclusive basis.

Once coupled and proven active, immobilized ligands are processed in an affinity chromatography approach to identify all the relevant targets and off-targets from a crude extract, which bind to this matrix. MS analysis of the identified protein spots and a parallel LC-MS/MS analysis permits detection of all the bound proteins (see Kinaxo homepage).

In combination with target-related biological assays, chemical proteomics can be instrumental in unraveling unknown cellular modes of action of the investigated compound. These data define new opportunities for drug development.

Using previously established chemistries, rationales for the generation of potent multitarget inhibitors directed against phylogenetically unrelated kinases could be implemented.